Page last updated: 2024-12-06

ly 178210

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

LY 178210: 5-hydroxytryptamine receptor agonist; structure given in first source; LY 228729 is the (-)-isomer; LY 228730 is the (+)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	60845
CHEMBL ID	296753
SCHEMBL ID	6364891
MeSH ID	M0182279

Synonyms (17)

Synonym
ly-228730
benz(cd)indole-6-carboxamide, 4-(dipropylamino)-1,3,4,5-tetrahydro-
114943-19-0
ly-178210
4-(dipropylamino)-1,3,4,5-tetrahydrobenz(cd)indole-6-carboxamide
ly 228729
ly 178210
CHEMBL296753 ,
L004509
4-(dipropylamino)-1,3,4,5-tetrahydrobenzo[cd]indole-6-carboxamide
SCHEMBL6364891
4-(di-n-propyl)amino-6-aminocarbonyl-1,3,4,5-tetrahydrobenz[cd]indole
YTOJFUORFUYGSV-UHFFFAOYSA-N
bdbm50227633
4-(dipropylamino)-1,3,4,5-tetrahydrobenzo[cd]indole-6-carboximidic acid
100561-24-8
DTXSID20905583

Research Excerpts

Bioavailability

Excerpt	Reference	Relevance
" Collectively, these results indicate that LY228729 is potent 5-HT1A agonist with bioavailability properties sufficient for clinical evaluation and with efficacy in preclinical models of anxiety, sexual disorders and motion sickness."	( Preclinical studies on LY228729: a potent and selective serotonin1A agonist. Benvenga, MJ; Calligaro, DO; Flaugh, ME; Foreman, MM; Fuller, RW; Leander, JD; Lucot, JB; Nelson, DL; Swanson, SP; Wong, DT, 1993)	0.29

Dosage Studied

Excerpt	Relevance	Reference
"LY228729 [(-)-4(dipropylamino)-1,3,4,5-tetrahydrobenz-[c,d]indole-6-carboxa mide]], an agonist at the 5-HT1A subtype of 5-HT receptor, was studied as an antiemetic in pigeons dosed with a highly emetic oncolytic agent, cyclophosphamide."	( Effects of a 5-HT1A receptor agonist on acute and delayed cyclophosphamide-induced vomiting. Leander, JD; Wolff, MC, 1997)	0.3

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (4)

Assay ID	Title	Year	Journal	Article
AID3665	Ability to inhibit binding of titreated serotonin to the 5-hydroxytryptamine 1 receptor in rat brain frontal cortex membranes	1988	Journal of medicinal chemistry, Sep, Volume: 31, Issue:9	6-substituted 1,3,4,5-tetrahydrobenz[cd]indol-4-amines: potent serotonin agonists.
AID5060	Ability to inhibit binding of titreated spiperone to the 5-hydroxytryptamine 2 receptor in rat brain frontal cortex membranes	1988	Journal of medicinal chemistry, Sep, Volume: 31, Issue:9	6-substituted 1,3,4,5-tetrahydrobenz[cd]indol-4-amines: potent serotonin agonists.
AID173458	Effect on 5HIAA (5-hydroxyindoleacetic acid) concentration in hypothalamus as an index of serotonin turnover in male Wistar rats expressed as percent of control	1988	Journal of medicinal chemistry, Sep, Volume: 31, Issue:9	6-substituted 1,3,4,5-tetrahydrobenz[cd]indol-4-amines: potent serotonin agonists.
AID174302	In vivo serum corticosterone concentration in male Wistar rats after injecting 0.3 mg/kg of compound subcutaneously	1988	Journal of medicinal chemistry, Sep, Volume: 31, Issue:9	6-substituted 1,3,4,5-tetrahydrobenz[cd]indol-4-amines: potent serotonin agonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	1 (10.00)	18.7374
1990's	7 (70.00)	18.2507
2000's	2 (20.00)	29.6817
2010's	0 (0.00)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.66

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

Metric	This Compound (vs All)
Research Demand Index	12.66 (24.57)
Research Supply Index	2.48 (2.92)
Research Growth Index	5.15 (4.65)
Search Engine Demand Index	0.00 (26.88)
Search Engine Supply Index	0.00 (0.95)

This Compound (12.66)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	11 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
8-hydroxy-2-(di-n-propylamino)tetralin 8-Hydroxy-2-(di-n-propylamino)tetralin: A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.. 8-OH-DPAT : A tetralin substituted at positions 1 and 7 by hydroxy and dipropylamino groups respectively	2.9	4	phenols; tertiary amino compound; tetralins	serotonergic antagonist
4-iodo-2,5-dimethoxyphenylisopropylamine 4-iodo-2,5-dimethoxyphenylisopropylamine: RN given refers to unlabeled parent cpd without isomeric designation; a serotonin agonist. 2-(4-iodo-2,5-dimethoxyphenyl)-1-methylethylamine : An organoiodine compound that is amphetamine bearing two methoxy substituents at positions 2 and 5 as well as an iodo substituent at position 4.	2	1	amphetamines; dimethoxybenzene; organoiodine compound
5-methoxytryptamine 5-Methoxytryptamine: Serotonin derivative proposed as potentiator for hypnotics and sedatives.. 5-methoxytryptamine : A member of the class of tryptamines that is the methyl ether derivative of serotonin.	2.04	1	aromatic ether; primary amino compound; tryptamines	5-hydroxytryptamine 2A receptor agonist; 5-hydroxytryptamine 2B receptor agonist; 5-hydroxytryptamine 2C receptor agonist; antioxidant; cardioprotective agent; human metabolite; mouse metabolite; neuroprotective agent; radiation protective agent; serotonergic agonist
alprazolam Alprazolam: A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238). alprazolam : A member of the class of triazolobenzodiazepines that is 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine carrying methyl, phenyl and chloro substituents at positions 1, 6 and 8 respectively. Alprazolam is only found in individuals that have taken this drug.	1.99	1	organochlorine compound; triazolobenzodiazepine	anticonvulsant; anxiolytic drug; GABA agonist; muscle relaxant; sedative; xenobiotic
diazepam Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5.	1.99	1	1,4-benzodiazepinone; organochlorine compound	anticonvulsant; anxiolytic drug; environmental contaminant; sedative; xenobiotic
nan 190 1-(2-methoxyphenyl)-4-(4-(2-phthalimido)butyl)piperazine: RN from Toxlit. NAN 190 : An N-alkylpiperazine that consists of (2-methoxyphenyl)piperazine in which the amine hydrogen is substituted by a 4-(2-phthalimido)butyl group.	2	1	N-alkylpiperazine; N-arylpiperazine; phthalimides	serotonergic antagonist
4-(2'-methoxyphenyl)-1-(2'-(n-(2''-pyridinyl)-4-iodobenzamido)ethyl)piperazine 4-(2'-methoxyphenyl)-1-(2'-(N-(2''-pyridinyl)-4-iodobenzamido)ethyl)piperazine: a 5-HT(1A) ligand; structure in first source	2	1
ritanserin Ritanserin: A selective and potent serotonin-2 antagonist that is effective in the treatment of a variety of syndromes related to anxiety and depression. The drug also improves the subjective quality of sleep and decreases portal pressure.. ritanserin : A thiazolopyrimidine that is 5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one which is substituted at position 7 by a methyl group and at position 6 by a 2-{4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl}ethyl group. A potent and long-acting seratonin (5-hydroxytryptamine, 5-HT) antagonist of the subtype 5-HT2 (Ki = 0.39 nM), it is used in the treatment of a variety of disorders including anxiety, depression and schizophrenia. It has little sedative action.	2	1	organofluorine compound; piperidines; thiazolopyrimidine	antidepressant; antipsychotic agent; anxiolytic drug; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; serotonergic antagonist
sumatriptan Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.. sumatriptan : A sulfonamide that consists of N,N-dimethyltryptamine bearing an additional (N-methylsulfamoyl)methyl substituent at position 5. Selective agonist for a vascular 5-HT1 receptor subtype (probably a member of the 5-HT1D family). Used (in the form of its succinate salt) for the acute treatment of migraine with or without aura in adults.	2	1	sulfonamide; tryptamines	serotonergic agonist; vasoconstrictor agent
corticosterone [no description available]	1.98	1	11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone	human metabolite; mouse metabolite
alpha-aminopyridine alpha-aminopyridine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #485. aminopyridine : Compounds containing a pyridine skeleton substituted by one or more amine groups.	2	1
colforsin Colforsin: Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.	1.97	1	acetate ester; cyclic ketone; labdane diterpenoid; organic heterotricyclic compound; tertiary alpha-hydroxy ketone; triol	adenylate cyclase agonist; anti-HIV agent; antihypertensive agent; plant metabolite; platelet aggregation inhibitor; protein kinase A agonist
gepirone gepirone: RN given refers to parent cpd; structure given in first source	1.98	1	N-arylpiperazine
gr 127935 GR 127935: a 5-HT 1D receptor antagonist. GR 127935 : A member of the class of benzamides obtained by formal condensation of the carboxy group of 2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-carboxylic acid and the anilino group of 4-methoxy-3-(4-methylpiperazin-1-yl)aniline. Potent and selective 5-HT1B/1D receptor antagonist (pKi values are 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptors). Displays > 100-fold selectivity over 5HT1A, 5-HT2A, 5-HT2C receptors and other receptor types. Centrally active following oral administration.	2	1	1,2,4-oxadiazole; benzamides; N-alkylpiperazine; N-arylpiperazine
bay r 1531 Bay R 1531: serotonin-1a receptor agonist	1.97	1
ergoline Ergolines: A series of structurally-related alkaloids that contain the ergoline backbone structure.. ergoline : An indole alkaloid whose structural skeleton is found in many naturally occurring and synthetic ergolines which are known to bind to neurotransmitter receptors, such as dopamine, noradrenaline and serotonin receptors and function as unselective agonists or antagonists at these receptors.	3.6	9	diamine; ergoline alkaloid; indole alkaloid fundamental parent; indole alkaloid; organic heterotetracyclic compound
oxadiazoles Oxadiazoles: Compounds containing five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom which exist in various regioisomeric forms.	2	1

Condition	Relationship Strength	Studies
Delayed Effects, Prenatal Exposure [description not available]	2.42	2
Anxiety Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.	2.04	1
Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.	2.42	2
Emesis [description not available]	2.39	2
Vomiting The forcible expulsion of the contents of the STOMACH through the MOUTH.	2.39	2
Depression, Endogenous [description not available]	1.99	1
Depressive Disorder An affective disorder manifested by either a dysphoric mood or loss of interest or pleasure in usual activities. The mood disturbance is prominent and relatively persistent.	1.99	1
Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	2	1

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